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Complicaciones y oportunidades pasadas por alto en el desarrollo de fármacos basados en péptidos macrobicíclicos: el

Isabelle J Smith¹, Simon M Popovic¹, John A Gladysz¹

¹Department of Chemistry, Texas A&M University, PO Box 30012, College Station, Texas 77842-3012, United States.

Journal of the American Chemical Society

|February 26, 2026

Abstract:

Many macrobicyclic compounds can undergo a widely overlooked conformational process, homeomorphic isomerization, that effectively turns molecules inside-out and leads to species with in,in, out,out, in,out, and out,in bridgeheads. Different chemical and biological properties would be expected. Some foundational aspects of this phenomenon are briefly reviewed, with both model compounds of the formula E((CH₂)_n)₃E (n ≥ 10, E = P, As, etc.) and macrobicyclic peptides. Attempts are made to bridge the differing cultural perspectives of the physical organic and chemical biology communities regarding bicyclic molecules. Opportunities are presented for (1) improving the stereochemical definition of macrobicyclic peptides and their adducts with proteins, (2) new drug design and efficacy protocols, and (3) refining or circumventing existing patented IP.

Palabras clave:

isomerización homeomórfica péptidos macrobicíclicos diseño de fármacos estereoquímica propiedad intelectual

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